AR061974A1 - Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion - Google Patents

Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion

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Publication number
AR061974A1
AR061974A1 ARP070103098A ARP070103098A AR061974A1 AR 061974 A1 AR061974 A1 AR 061974A1 AR P070103098 A ARP070103098 A AR P070103098A AR P070103098 A ARP070103098 A AR P070103098A AR 061974 A1 AR061974 A1 AR 061974A1
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AR
Argentina
Prior art keywords
alkyl
amino
optionally substituted
hydroxyl
positions
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ARP070103098A
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English (en)
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Novartis Ag
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Priority claimed from EP06117227A external-priority patent/EP1878733A1/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR061974A1 publication Critical patent/AR061974A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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Abstract

También se describen composiciones farmacéuticas que contienen los compuestos, y procesos para la preparación de los compuestos. Reivindicación 1: Un compuesto de la fórmula (1), en forma libre o de sal de solvato, en donde: T¹ es un grupo heterocíclico de 4 a 14 miembros opcionalmente sustituido en una, dos o tres posiciones por R¹, alcoxilo C₁₋₈, cicloalquilo C₃₋₅, tioalquilo C₁₋₈, halógeno, halo-alquilo C₁₋₈, amino, alquilo C₁₋₈-amino, di-(alquilo C₁₋₈)-amino, ciano, oxo, hidroxilo, carboxilo, o nitro; T² es un grupo heterocíclico de 4 a 14 miembros opcionalmente sustituido en una, dos, o tres posiciones de R¹, R², R⁵, alcoxilo C₁₋₈, alcoxilo C₁₋₈-carbonilo, tioalquilo C₁₋₈, halógeno, haloalquilo C₁₋₈, amino, alquilo C₁₋₈-amino, di-(alquilo C₁₋₈)-amino, ciano, oxo, hidroxilo, carboxilo o nitro; cualquiera de Rᵃ y Rᵇ son independientemente hidrógeno; alquilo C₁₋₈ opcionalmente sustituido en una, dos o tres posiciones por R⁴; cicloalquilo C₃₋₁₀ opcionalmente sustituido en una o dos posiciones por hidroxilo, amino, alquilo C₁₋₈, alcoxilo C₁₋₈, halógeno, ciano, oxo, carboxilo o nitro; o arilo C₆₋₁₅ opcionalmente sustituido en una, dos o tres posiciones por halógeno, hidroxilo, amino, ciano, oxo, carboxilo, nitro o R⁵; R¹ es alquilo C₁₋₈, alquenilo C₂₋₈, o alquinilo C₂₋₈ opcionalmente sustituido en una, dos o tres posiciones por hidroxilo, ciano, amino o halógeno; R² es arilo C₆₋₁₅ opcionalmente sustituido en una, dos o tres posiciones por halógeno, hidroxilo, R¹, R⁵, tioalquilo C₁₋₈, amino, alquilo C₁₋₈-amino, di-(alquilo C₁₋₈)-amino, ciano, carboxilo, nitro, -O-arilo C₆₋₁₅, halo-alquilo C₁₋₈, -NR⁶R⁷, alquilo C₁₋₈-NR⁶R⁷, -O-alquilo C₁₋₈-NR⁶R⁷, -alquilo C₁₋₈-R⁵, -O-R¹, -O-R⁵, -C(=O)-R⁵, -C(=O)-NH₂, -C(=O)NR⁶R⁷, -C(=O)-O-R¹, -O-C(=O)-R¹, -SO₂-NH₃, -SO₂-R¹, -NH-SO₂-alquilo C₁₋₈, -C(=O)-NH-R⁵, -SO₂-arilo C₆₋₁₅, -SO₂-R⁵, -SO₂NR⁶R⁷, o por alcoxilo C₁₋₈ opcionalmente sustituido en una posición por di-(alquilo C₁₋₈)-amino; R⁴ es hidroxilo, amino, alcoxilo C₁₋₈, tioalquilo C₁₋₈, halógeno, halo-alquilo C₁₋₈, alquilo C₁₋₈-amino, di(alquilo C₁₋₈)-amino, ciano, carboxilo, nitro, -N(H)-C(=NH)-NH₂, -N(H)-SO₂-R², -R², -C(=O)-R², -C(=O)-R⁵, -O-R², -O-R⁵, -N(H)-R⁵, -N(H)-R², -NR⁶R⁷, -C(=O)-R¹, -C(=O)-NH₂, -SO₂-R⁵, -C(=O)-O-R¹, -C(=O)-OR², -C(=O)-O-R⁵, -SO₂-R² o -C(=O)-N(H)-alquilo C₁₋₈-C(=O)-N(H)-R²; o R⁴ es un grupo heterocíclico de 4 a 14 miembros, estando este grupo opcionalmente sustituido en una, dos o tres posiciones por hidroxilo, halógeno, oxo, ciano, amino, alquilo C₁₋₈-amino, di-(alquilo C₁₋₈)-amino, carboxilo, nitro, -N(H)R¹, -N(H)-SO₂-alquilo C₁₋₈, -N(H)-C(=O)-alquilo C₁₋₄-R², C(=O)-NH₂, -C(=O)-NR⁶R⁷, -C(=O)-N(H)-alquilo C₁₋₈-R⁶, -C(=O)-R², -C(=O)-R⁵, alcoxilo C₁₋₈, tioalquilo C₁₋₈, cicloalquilo C₃₋₁₀, -C(=O)-R¹, halo-alquilo C₁₋₈, -R², -alquilo C₁₋₈-R², -R⁵, -SO₂-alquilo C₁₋₈, -SO₂-R², -SO₂-R⁵, o -SO₂NR⁶R⁷, o por alquilo C₁₋₈ opcionalmente sustituido en una posición por hidroxilo; o R⁴ es arilo C₆₋₁₅ opcionalmente sustituido en una, dos o tres posiciones por hidroxilo, alcoxilo C₁₋₈, -O-arilo C₆₋₁₅, o por alquilo C₁₋₈ opcionalmente sustituido en una posición por hidroxilo; o R⁴ es cicloalquilo C₃₋₁₀ sustituido en una, dos o tres posiciones por hidroxilo, amino, halógeno, ciano, carboxilo, nitro o alquilo C₁₋₈; R⁵ es un grupo heterocíclico de 4 a 14 miembros opcionalmente sustituido en una, dos o tres posiciones por oxo, amino, halógeno, alquilo C₁₋₈-amino, di-(alquilo C₁₋₈)-amino, ciano, hidroxilo, carboxilo, nitro, -NR¹, alcoxilo C₁₋₈, tioalquilo C₁₋₈, halo-alquilo C₁₋₈, -C(=O)-NH₂, o SO₂-NH₂; y R⁶ y R⁷ son independientemente hidrógeno, -R¹, alquilo C₁₋₈-amino, di-(alquilo C₁₋₈)-amino, arilo C₆₋₁₅, -alquilo C₁₋₈-arilo C₆₋₁₅, R⁵, ó alquilo C₁₋₈-R⁵; en el entendido de que, cuando R¹ es piridin-2-ilo, T² es piridin-3-ilo, y Rᵃ es hidrógeno, entonces Rᵇ no es 2-(1H-indol-3-il)-etilo.
ARP070103098A 2006-07-14 2007-07-12 Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion AR061974A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06117227A EP1878733A1 (en) 2006-07-14 2006-07-14 Pyrimidine derivatives as ALK-5 inhibitors
EP06119564 2006-08-25

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AR061974A1 true AR061974A1 (es) 2008-08-10

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US (1) US7989458B2 (es)
EP (1) EP2044056B1 (es)
JP (1) JP4960450B2 (es)
KR (1) KR101172936B1 (es)
AR (1) AR061974A1 (es)
AU (1) AU2007271964B2 (es)
BR (1) BRPI0714409A2 (es)
CA (1) CA2657227A1 (es)
CL (1) CL2007002043A1 (es)
ES (1) ES2393932T3 (es)
MX (1) MX2009000310A (es)
PE (1) PE20080944A1 (es)
PL (1) PL2044056T3 (es)
PT (1) PT2044056E (es)
RU (1) RU2485115C2 (es)
TW (1) TW200821297A (es)
WO (1) WO2008006583A1 (es)

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